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K-858

Cat. No. M7876

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K-858 Structure
Synonym:

K858 Racemic

Size Price Availability Quantity
5mg USD 40  USD40 In stock
10mg USD 66  USD66 In stock
25mg USD 132  USD132 In stock
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Biological Activity

K858 (Racemic) is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM. Eg5 is a key protein involved in the formation of bipolar spindles. K858 induces mitotic arrest, caspase-3 activation and cell growth inhibition in HCT116 cells. K858 (5 μM) induces mitotic cell death in cancer cells but not in normal cells. K858 (1, 10, 100 μM) inhibits the MCF7, BT474 and SKBR3 cell lines, and only at 10 and 100 μM suppresses MDA-MB231 cell line after treatment for 24 h. K858 incereases Bax/Bcl2 RNA ratio and survivin in the four cell lines.

Chemical Information
Molecular Weight 277.34
Formula C13H15N3O2S
CAS Number 72926-24-0
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Sandeep K Talapatra, et al. Crystal structure of the Eg5 - K858 complex and implications for structure-based design of thiadiazole-containing inhibitors

[2] Sabrina Giantulli, et al. Growth arrest and apoptosis induced by kinesin Eg5 inhibitor K858 and by its 1,3,4-thiadiazoline analogue in tumor cells

[3] Ludovica Taglieri, et al. The kinesin Eg5 inhibitor K858 induces apoptosis and reverses the malignant invasive phenotype in human glioblastoma cells

[4] Francesca De Iuliis, et al. The kinesin Eg5 inhibitor K858 induces apoptosis but also survivin-related chemoresistance in breast cancer cells

[5] Ryuichiro Nakai, et al. K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells

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Keywords: K-858, K858 Racemic supplier, Kinesin, inhibitors, activators

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